During the past decade, treatment with cyclosporine, an immunosuppressive agent, has contributed substantially to enhanced allograft and patient survival after liver transplantation. Currently, the 1-year survival rate after liver transplantation is more than 80% in major liver transplantation centers, in contrast with approximately 60% before the availability of cyclosporine. Its predominant immunologic effect is inhibition of lymphokine production and secretion by helper T cells. The use of cyclosporine, however, is associated with numerous adverse effects, the most important of which are nephrotoxicity, hypertension, neurotoxicity, opportunistic infections, and malignant lesions. Acute nephrotoxicity, hypertension, and neurotoxicity usually can be reversed by decreasing the dose of cyclosporine. Measurement of cyclosporine concentrations in the blood is essential for optimization of immunosuppressive therapy and prevention of toxicity.